Amino acid and peptide esters of abacavir: synthesis and activity against human immunodeficiency virus type 1 in cell culture
- First Online:
- Cite this article as:
- Stankova, I., Stanoeva, K., Hinkov, A. et al. Med Chem Res (2012) 21: 4053. doi:10.1007/s00044-011-9956-y
- 216 Downloads
Abacavir (ABC) is clinically associated with hypersensitivity reactions, risk for cardiovascular disease, etc. A possible way to minimize side effects is by modifying chemical structure. Three esters of ABC containing amino acid (glycine) and dipeptide esters (glycyl-glycine) were synthesized and their activity on HIV-1 III B replication in MT-4 cells was evaluated. One of the newly synthesized esters—Gly-ABC—demonstrates low-cytotoxicity and high-anti-HIV-1 activity in MT-4 cells, as well as low-mitochondrial toxicity and high-genetic barrier to resistance.